EP1453512B8 - Derives d'acetylene possedant une activite antagoniste mglur 5 - Google Patents

Derives d'acetylene possedant une activite antagoniste mglur 5 Download PDF

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Publication number
EP1453512B8
EP1453512B8 EP02792867A EP02792867A EP1453512B8 EP 1453512 B8 EP1453512 B8 EP 1453512B8 EP 02792867 A EP02792867 A EP 02792867A EP 02792867 A EP02792867 A EP 02792867A EP 1453512 B8 EP1453512 B8 EP 1453512B8
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EP
European Patent Office
Prior art keywords
mglur
antagonistic activity
acetylene derivatives
acetylene
derivatives
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
EP02792867A
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German (de)
English (en)
Other versions
EP1453512A1 (fr
EP1453512B1 (fr
Inventor
Fabrizio Gasparini
Yves Auberson
Silvio Ofner
Terance W. Hart
Kaspar Zimmermann
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Novartis AG
Original Assignee
Novartis Pharma GmbH
Novartis AG
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Filing date
Publication date
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Application filed by Novartis Pharma GmbH, Novartis AG filed Critical Novartis Pharma GmbH
Priority to SI200230385T priority Critical patent/SI1453512T1/sl
Publication of EP1453512A1 publication Critical patent/EP1453512A1/fr
Application granted granted Critical
Publication of EP1453512B1 publication Critical patent/EP1453512B1/fr
Publication of EP1453512B8 publication Critical patent/EP1453512B8/fr
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/24—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/08—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms with acylated ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
EP02792867A 2001-12-04 2002-12-03 Derives d'acetylene possedant une activite antagoniste mglur 5 Expired - Lifetime EP1453512B8 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
SI200230385T SI1453512T1 (sl) 2001-12-04 2002-12-03 Derivati etina z antagonisticnim delovanjem na MGLUR 5

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0128996.6A GB0128996D0 (en) 2001-12-04 2001-12-04 Organic compounds
GB0128996 2001-12-04
PCT/EP2002/013670 WO2003047581A1 (fr) 2001-12-04 2002-12-03 Derives d'acetylene possedant une activite antagoniste mglur 5

Publications (3)

Publication Number Publication Date
EP1453512A1 EP1453512A1 (fr) 2004-09-08
EP1453512B1 EP1453512B1 (fr) 2006-05-31
EP1453512B8 true EP1453512B8 (fr) 2006-07-19

Family

ID=9926969

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02792867A Expired - Lifetime EP1453512B8 (fr) 2001-12-04 2002-12-03 Derives d'acetylene possedant une activite antagoniste mglur 5

Country Status (32)

Country Link
US (4) US7348353B2 (fr)
EP (1) EP1453512B8 (fr)
JP (2) JP4176020B2 (fr)
KR (2) KR100980901B1 (fr)
CN (2) CN101366714B (fr)
AR (2) AR037682A1 (fr)
AT (1) ATE327755T1 (fr)
AU (1) AU2002358585B2 (fr)
BR (1) BR0214666A (fr)
CA (1) CA2466560C (fr)
CO (1) CO5590929A2 (fr)
CY (1) CY1105460T1 (fr)
DE (1) DE60211944T2 (fr)
DK (1) DK1453512T3 (fr)
EC (1) ECSP045139A (fr)
EG (1) EG24936A (fr)
ES (1) ES2263842T3 (fr)
GB (1) GB0128996D0 (fr)
HK (1) HK1071510A1 (fr)
HU (1) HU229429B1 (fr)
IL (1) IL161990A0 (fr)
MX (1) MXPA04005456A (fr)
MY (1) MY137774A (fr)
NO (1) NO327005B1 (fr)
NZ (1) NZ533266A (fr)
PE (1) PE20030640A1 (fr)
PL (1) PL212996B1 (fr)
PT (1) PT1453512E (fr)
RU (1) RU2341515C2 (fr)
TW (1) TWI328578B (fr)
WO (1) WO2003047581A1 (fr)
ZA (1) ZA200403713B (fr)

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GB0325956D0 (en) * 2003-11-06 2003-12-10 Addex Pharmaceuticals Sa Novel compounds
EP2305352A1 (fr) 2004-04-02 2011-04-06 Merck Sharp & Dohme Corp. Inhibiteurs de la 5-alpha-reductase pour le traitement d'hommes aux troubles métaboliques et anthropométriques
GB0503646D0 (en) * 2005-02-22 2005-03-30 Novartis Ag Organic compounds
GB0508318D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508314D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0508319D0 (en) * 2005-04-25 2005-06-01 Novartis Ag Organic compounds
GB0514296D0 (en) * 2005-07-12 2005-08-17 Novartis Ag Organic compounds
JP2010502664A (ja) 2006-09-11 2010-01-28 ノバルティス アクチエンゲゼルシャフト 代謝型グルタミン酸受容体の調節剤としてのニコチン酸誘導体
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
AU2008261102B2 (en) 2007-06-04 2013-11-28 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
BRPI0818560A2 (pt) * 2007-10-12 2019-09-24 Novartis Ag compostos orgânicos
AU2012254934B2 (en) * 2007-10-12 2013-10-17 Novartis Ag Metabotropic glutamate receptor modulators for the treatment of Parkinson's disease
CA2930674A1 (fr) 2008-06-04 2009-12-10 Synergy Pharmaceuticals Inc. Agonistes de guanylate cyclase utile dans le traitement de troubles gastro-intestinaux, d'une inflammation, d'un cancer et d'autres troubles
WO2010000763A2 (fr) * 2008-06-30 2010-01-07 Novartis Ag Produits de combinaison
MX2011001664A (es) * 2008-08-12 2011-03-25 Novartis Ag Procesos para la preparacion del metil-ester del acido 4-oxo-octahidro-indol-1-carbociclico y derivados del mismo.
US8334287B2 (en) 2009-07-17 2012-12-18 Hoffmann-La Roche Inc. Imidazoles
CN102573842A (zh) 2009-07-23 2012-07-11 诺瓦提斯公司 氮杂双环烷基衍生物或吡咯烷-2-酮衍生物的用途
JO3250B1 (ar) 2009-09-22 2018-09-16 Novartis Ag إستعمال منشطات مستقبل نيكوتينيك أسيتيل كولين ألفا 7
EP2490691A1 (fr) 2009-10-20 2012-08-29 Novartis AG Utilisation de 1h-quinazoline-2,4-diones
PE20130213A1 (es) * 2010-04-30 2013-03-19 Novartis Ag Marcadores predictivos utiles en el tratamiento del sindrome fragil x (fxs)
KR20130098181A (ko) 2010-06-24 2013-09-04 노파르티스 아게 1ｈ-퀴나졸린-2,4-디온의 용도
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
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US9067881B2 (en) 2011-01-24 2015-06-30 Novartis Ag 4-tolyl-ethynyl-octahydro-indole-1-ester derivatives
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CN103889427A (zh) 2011-09-07 2014-06-25 诺华股份有限公司 1h-喹唑啉-2,4-二酮用于预防或治疗光敏性癫痫的应用
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GB201215033D0 (en) 2012-08-23 2012-10-10 Novartis Ag Diazepinone derivatives
WO2014111751A1 (fr) 2013-01-15 2014-07-24 Novartis Ag Utilisation d'agonistes du récepteur nicotinique alpha 7 pour le traitement de la narcolepsie
CA2898045C (fr) 2013-01-15 2018-08-28 Novartis Ag Utilisation d'agonistes des recepteurs nicotiniques de l'acetylcholine alpha 7
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JP6606491B2 (ja) 2013-06-05 2019-11-13 シナジー ファーマシューティカルズ インコーポレイテッド グアニル酸シクラーゼｃの超高純度アゴニスト、その作成および使用方法
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EP1453512A1 (fr) 2004-09-08
CN101366714A (zh) 2009-02-18
KR20100020044A (ko) 2010-02-19
CA2466560A1 (fr) 2003-06-12
DE60211944T2 (de) 2007-05-16
AR088921A2 (es) 2014-07-16
PL368739A1 (en) 2005-04-04
AU2002358585B2 (en) 2006-01-19
MY137774A (en) 2009-03-31
KR100959204B1 (ko) 2010-05-19
PE20030640A1 (es) 2003-09-12
KR20050044657A (ko) 2005-05-12
DK1453512T3 (da) 2006-08-28
NZ533266A (en) 2005-02-25
BR0214666A (pt) 2004-11-03
ECSP045139A (es) 2004-07-23
PL212996B1 (pl) 2012-12-31
KR100980901B1 (ko) 2010-09-07
US20120010263A1 (en) 2012-01-12
JP5036648B2 (ja) 2012-09-26
TW200304910A (en) 2003-10-16
PT1453512E (pt) 2006-10-31
JP2005514381A (ja) 2005-05-19
CN100430059C (zh) 2008-11-05
CY1105460T1 (el) 2010-04-28
CN1592623A (zh) 2005-03-09
CN101366714B (zh) 2014-09-17
RU2004120781A (ru) 2006-01-10
NO20042673L (no) 2004-06-25
JP4176020B2 (ja) 2008-11-05
JP2008303226A (ja) 2008-12-18
ES2263842T3 (es) 2006-12-16
HUP0402191A3 (en) 2010-03-29
US20050065191A1 (en) 2005-03-24
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HU229429B1 (en) 2013-12-30
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US8536229B2 (en) 2013-09-17
US20080146647A1 (en) 2008-06-19
MXPA04005456A (es) 2004-10-11
ATE327755T1 (de) 2006-06-15
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US7348353B2 (en) 2008-03-25
RU2341515C2 (ru) 2008-12-20
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HK1071510A1 (en) 2005-07-22
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EP1453512B1 (fr) 2006-05-31

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